The Keap1-Nrf2 pathway is the major regulator of cytoprotective responses to oxidative and electrophilic stress.Although cytoprotection provided by Nrf2 activation is important for cancer chemoprevention in normal and premalignant tissues, in fully malignant cells Nrf2 activity provides growth advantage by increasing cancer chemoresistance and enhancing tumor cell growth Given that high Nrf2 activity commonly occurs in cancer cells with adverse outcomes, there is a need for therapies to inhibit Nrf2. Unfortunately, due to structural similarity with some other bZip family members, the development of specific Nrf2 inhibitors is a challenging task and only a few studies of Nrf2 inhibition have been published to date.

References

1.Emilia Kansanen et al. Redox Biology Volume 1, Issue 1, 2013, Pages 45-49